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BAY-3827

CAS No. : 2377576-35-5

MCE 国际站：BAY-3827

产品活性：BAY-3827 是强效的、选择性的 AMPK 抑制剂，IC₅₀ 值为 1.4 nM (10 M ATP) 和 15 nM (2 mM ATP)。BAY-3827 对其他 331 种被测激酶的选择性超过 500 倍相比于 AMPK。AMPK 抑制乙酰 CoA 羧化酶 1 的磷酸化，并在雄激素依赖的前列腺癌细胞株中显示出强效的抗增殖活性。

研究领域：Epigenetics | PI3K/Akt/mTOR

作用靶点：AMPK

In Vitro: BAY-3827 (0-200 µM) inhibits AMPK kinase activity with IC₅₀ values of 1.4 nM at low, 10 M ATP concentration ａnd 15 nM at high, 2 mM ATP concentration.
BAY-3827 (0-200 µM) inhibits Aurora A, Flt3, c-Met ａnd Rsk4 with IC₅₀ values of 1324, 124, 788 ａnd 36 nM , respectively with 10 M ATP concentration.
BAY-3827 (overnight) strongly reduces ACC1 Ser79 phosphorylation in LNCaP ａnd VCaP cells, ａnd shows a lesser extent in IMR-32 ａnd especially in Colo320 cells.
BAY-3827 (0-10 nM; 6 d) shows strong inhibitory effects to LNCaP ａnd VCaP cells.
BAY-3827 (1 ａnd 5 µM; 24 ａnd 48 h) represses LIPE gene expression, reduces serine/threonine kinase AKT3 ａnd blocks the expression of several genes from the mitochondrial carnitine palmitoyltransferase (CPT) family which is involved in acyl carnitine formation in VCaP cells.
BAY-3827 (5 µM; 2-4 d) significantly increases the formation of lipid droplets in comparison to androgen treatment only.

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